CO2 utilization as a supercritical solvent and supercritical antisolvent in production of sertraline hydrochloride nanoparticles

Abstract

Supercritical fluid (SCF) processes have attracted great attention for fabricating micro and nanoparticles in the pharmaceutical applications. Herein we utilized, for the first time, Gas Anti-Solvent (GAS) and Rapid Expansion of Supercritical Solution with Solid Cosolvent (RESS-SC) processes to fabricate nanoparticles of sertraline hydrochloride (SRT), a widespread antidepressant. Design of experiment (DoE) was implemented to evaluate the influences of various operating conditions and find an optimal combination of the conditions to achieve the smallest particle size (PS). Variations of the physical and chemical properties were studied by performing FTIR, FESEM, DLS, XRD, and DSC analyses as well as dissolution rate tests. By reducing the particle size from about 50 μm to 102 ± 11 nm at low pressures, the results showed the superiority of GAS compared to RESS-SC with a minimum particle size of 185 ± 9 nm. Furthermore, the GAS and RESS-SC methods led to dissolution rates that were 50 and 18 times greater than that of the original SRT, respectively.